title: Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics.
abstract: The discovery and initial optimization of a novel anthranilic acid derived class of antibacterial agents has been described in a recent series of papers. This paper describes the discovery of 1-acylindazol-3-ols as a novel bioisostere of an anthranilic acid. The synthesis and structure-activity relationships of the indazol bioisosteres are described herein.
authors.affiliation: Medicinal Chemistry, 301 Henrietta Street, Kalamazoo, MI 49001, USA.
authors.forename: Cory
authors.initials: C
authors.lastname: Stiff
authors.forename: David R
authors.initials: DR
authors.lastname: Graber
authors.forename: Atli
authors.initials: A
authors.lastname: Thorarensen
authors.forename: Brian D
authors.initials: BD
authors.lastname: Wakefield
authors.forename: Keith R
authors.initials: KR
authors.lastname: Marotti
authors.forename: Earline P
authors.initials: EP
authors.lastname: Melchior
authors.forename: Michael T
authors.initials: MT
authors.lastname: Sweeney
authors.forename: Fusen
authors.initials: F
authors.lastname: Han
authors.forename: Douglas C
authors.initials: DC
authors.lastname: Rohrer
authors.forename: Gary E
authors.initials: GE
authors.lastname: Zurenko
authors.forename: Donna L
authors.initials: DL
authors.lastname: Romero
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D018360:Crystallography, X-Ray; D007191:Indazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015394:Molecular Structure; D014176:Protein Biosynthesis / Q000187:drug effects*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D007191:Indazoles; D062367:ortho-Aminobenzoates